Epidermal Growth Factor Receptor



Epidermal Growth Factor Receptor (EGFR or ERBB1) is found on the cell surface and associates to homodimers upon binding of its ligands such as the Epidermal Growth Factor (EGF) to its extracellular domain. The dimerization stimulates autophosphorylation of several tyrosine residues in the intracellular kinase domain which signal downstream transduction cascades. A human EGFR-2 (HER-2 or ERBB2) is involved in beast cancer. ERBB3 uses neuregulin as a ligand. ERBB4 is a closely related receptor tyrosine kinase. The images at the left and at the right correspond to one representative EGFR, i.e. crystal structure of unliganded Drosophila Epidermal Growth Factor Receptor ectodomain (3i2t).

3D Structures of Epidermal Growth Factor Receptor
Update June 2011

EGFR extracellular domain
3ltf – DmEGFR extracellular domain+spitz protein – Drosophila melanogaster

3i2t - DmEGFR extracellular domain

3n85 – hERBB2 extracellular domain+FAB37 light and heavy chains – human

1yy9 – hERBB1 extracellular domain+antibody

1m6b – hERBB3 extracellular domain

1mox - hEGFR extracellular domain+TGF alpha

1ivo, 1nql, 3njp - hEGFR extracellular domain+hEGF

3ltg - EGFR extracellular domain+ Spitz (mutant) – Drosophila melanogaster

EGFR transmembrane domain
2ks1 – hERBB1+hERBB2 transmembrane domains

EGFR kinase domain
3gt8 – hEGFR kinase domain+peptide+AMPPNP

2qs2 – hERBB1 kinase domain

2gs6 - hERBB1 kinase domain+peptide

2gs7 - hERBB1 kinase domain+AMPPNP

2eb2, 2jit, 1m14 – hERBB1 kinase domain (mutant)

2jiu, 2jiv, 2ito, 2itp, 2itq, 2itt, 2itu, 2itw, 2itz, 2j6m, 2j5e, 2j5f, 1m17 - hERBB1 kinase domain (mutant)+inhibitor

2rf9, 2rfd, 2rfe, 1xkk, 3lzb, 3poz - hERBB1 kinase domain+inhibitor

2eb3, 2itn, 2itv, 2itx, 2ity - hERBB1 kinase domain (mutant)+AMPPNP

3b2u - hERBB1 kinase domain+IMC-11F8 FAB fragment

3kex – hERBB3 kinase domain

EGFR juxtamembrane domain
3gop – hERBB1 kinase and juxtamembrane domains

1z9i - hERBB1 juxtamembrane domain

EGFR fragments
3i7z – hEGFR fragment+hTyrosine phosphatase

3g5v, 3g5y, 3g5z, 3g5x – EGFR fragment+antibody – mouse

3ika – hERBB1 (mutant)+inhibitor

2rgp – hERBB1+hydrazone

3bel – hERBB1+oxime

3c09 – hERBB1 domain III+antibody

2b2u, 3b2v – hERBB1 fragment+antibody

3buo – EGFR 13-mer+hCBL N-terminal

Additional Resources
For additional information, see: Cancer